GSK269962A (GSK 269962) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A has anti-inflammatory and vasodilatory activities.
IC50&Target
ROCK1
1.6 nM (IC50)
ROCK2
4 nM (IC50)
RSK1
132 nM (IC50)
MSK1
49 nM (IC50)
AKT1
955 nM (IC50)
AKT2
1350 nM (IC50)
AKT3
1510 nM (IC50)
CDK2
3500 nM (IC50)
GSK3α
1260 nM (IC50)
体外研究
GSK269962A has an IC50 of 1.6 nM toward recombinant human ROCK1. GSK269962A exhibits more than 30-fold selectivity against a panel of serine/threonine kinases.
GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM.
体内研究
GSK269962A is a potent antihypertensive agent. GSK269962A (0.3, 1, and 3 mg/kg; oral gavage) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial.
Animal Model:
Male Sprague-Dawley rats (350-400g)
Dosage:
0.3, 1, and 3 mg/kg
Administration:
Oral gavage; 12 hours
Result:
Induced a dose-dependent reduction in blood pressure.
分子式
C29H30N8O5
分子量
570.60
CAS号
850664-21-0
运输条件
Room temperature in continental US; may vary elsewhere.